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ACS Med Chem Lett. 2013 May 17;4(7):612-5. doi: 10.1021/ml4001529. eCollection 2013 Jul 11.

C-Glucopyranosyl-1,2,4-triazoles As New Potent Inhibitors of Glycogen Phosphorylase.

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Department of Organic Chemistry, University of Debrecen , POB 20, H-4010 Debrecen, Hungary.
Department of Medical Chemistry, Medical and Health Science Centre, University of Debrecen , Egyetem tér 1, H-4032 Debrecen, Hungary.


Glycogen phosphorylase inhibitors are considered as potential antidiabetic agents. 3-(β-d-Glucopyranosyl)-5-substituted-1,2,4-triazoles were prepared by acylation of O-perbenzoylated N (1)-tosyl-C-β-d-glucopyranosyl formamidrazone and subsequent removal of the protecting groups. The best inhibitor was 3-(β-d-glucopyranosyl)-5-(2-naphthyl)-1,2,4-triazole (K i = 0.41 μM against rabbit muscle glycogen phosphorylase b).


1,2,4-Triazole; C-glucopyranosyl derivative; bioisoster; glycogen phosphorylase; inhibitor

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